BR112015022861A2 - bromodomain inhibitors - Google Patents

bromodomain inhibitors

Info

Publication number
BR112015022861A2
BR112015022861A2 BR112015022861A BR112015022861A BR112015022861A2 BR 112015022861 A2 BR112015022861 A2 BR 112015022861A2 BR 112015022861 A BR112015022861 A BR 112015022861A BR 112015022861 A BR112015022861 A BR 112015022861A BR 112015022861 A2 BR112015022861 A2 BR 112015022861A2
Authority
BR
Brazil
Prior art keywords
bromodomain inhibitors
compounds
formula
diseases
aids
Prior art date
Application number
BR112015022861A
Other languages
Portuguese (pt)
Other versions
BR112015022861A8 (en
Inventor
Liu Dachun
S Sheppard George
H Holms James
K Pratt John
F Mcdaniel Keith
A Hasvold Lisa
Mantei Robert
D Fidanze Steven
Le Wang
Mcclellan William
Dai Yujia
Original Assignee
Abbvie Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Abbvie Inc filed Critical Abbvie Inc
Publication of BR112015022861A2 publication Critical patent/BR112015022861A2/en
Publication of BR112015022861A8 publication Critical patent/BR112015022861A8/en

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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Abstract

resumo "inibidores de bromodomínio" a presente invenção refere-se a compostos de fórmula (i) (i) onde r1, r2, a1, a2, a3, a4, x, e y têm qualquer um dos valores definidos na especificação, e sais farmaceuticamente aceitáveis dos mesmos, que são úteis co-mo agentes no tratamento de doenças e condições, incluindo doenças inflamató-rias, câncer, e aids. são também fornecidas composições farmacêuticas compre-endendo um ou mais compostos de fórmula (i).Summary "Bromodomain Inhibitors" The present invention relates to compounds of formula (i) (i) wherein r1, r2, a1, a2, a3, a4, x, and y have any of the values defined in the specification, and pharmaceutically salts which are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).

BR112015022861A 2013-03-11 2014-03-11 bromodomain inhibitors BR112015022861A8 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361776530P 2013-03-11 2013-03-11
PCT/US2014/023437 WO2014164771A1 (en) 2013-03-11 2014-03-11 Bromodomain inhibitors

Publications (2)

Publication Number Publication Date
BR112015022861A2 true BR112015022861A2 (en) 2017-07-18
BR112015022861A8 BR112015022861A8 (en) 2019-11-26

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Country Link
US (1) US9050346B2 (en)
EP (1) EP2970262A1 (en)
JP (1) JP2016512524A (en)
CN (1) CN105164127A (en)
AU (1) AU2014249025A1 (en)
BR (1) BR112015022861A8 (en)
CA (1) CA2904048A1 (en)
MX (1) MX2015012005A (en)
WO (1) WO2014164771A1 (en)

Families Citing this family (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
JP2016507496A (en) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． Novel heterocyclic compounds as bromodomain inhibitors
EP3581576B1 (en) 2013-03-15 2022-01-26 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors for use in the treatment of a proliferative disease in combination with a janus kinase inhibitor
HUE049469T2 (en) 2013-06-21 2020-09-28 Zenith Epigenetics Ltd Novel bicyclic bromodomain inhibitors
EP3010918B1 (en) 2013-06-21 2018-08-15 Zenith Epigenetics Ltd. Novel substituted bicyclic compounds as bromodomain inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
KR20160038008A (en) 2013-07-31 2016-04-06 제니쓰 에피제네틱스 코포레이션 Novel quinazolinones as bromodomain inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
CN106414442B (en) 2014-04-23 2019-03-15 因赛特公司 1H- pyrrolo- [2,3-c] pyridine -7 (6H) -one and pyrazolo [3,4-c] pyridine -7 (6H) -one as BET protein inhibitor
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
CA2966303A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
WO2016090219A1 (en) * 2014-12-05 2016-06-09 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
JP2017538721A (en) 2014-12-17 2017-12-28 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． Bromodomain inhibitors
US10786519B2 (en) 2015-02-23 2020-09-29 Mayo Foundation For Medical Education And Research Methods and materials for treating human immunodeficiency virus infections
WO2016172194A1 (en) * 2015-04-20 2016-10-27 Mayo Foundation For Medical Education And Research Methods and materials for killing hiv infected cells
TWI732785B (en) * 2015-09-21 2021-07-11 美商普雷辛肯公司 Heterocyclic compounds and uses thereof
TW201722966A (en) 2015-10-29 2017-07-01 英塞特公司 Amorphous solid form of a BET protein inhibitor
AU2017251537B2 (en) * 2016-04-15 2020-10-08 Abbvie Inc. Bromodomain inhibitors
FI3472157T3 (en) 2016-06-20 2023-06-01 Incyte Corp Crystalline solid forms of a bet inhibitor
AU2017357329A1 (en) 2016-11-10 2019-06-13 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
CN108069959A (en) * 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application
CN108069958A (en) * 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 A kind of nitrogen-containing hetero cyclics, its preparation method, pharmaceutical composition and application
US20190367457A1 (en) 2016-12-30 2019-12-05 Mitobridge, Inc. Oxopyridine derivatives useful as aminocarboxymuconate semialdehyde decarboxylase (acmsd) inhibitors
GB201703282D0 (en) * 2017-03-01 2017-04-12 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
US20210130346A1 (en) * 2017-04-14 2021-05-06 Abbvie Inc. Bromodomain Inhibitors
GB201716392D0 (en) 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
KR20190043437A (en) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 Heterocylic compound as a protein kinase inhibitor
US11427593B2 (en) * 2018-01-16 2022-08-30 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Bromodomain inhibitor compound and use thereof
US11192900B2 (en) 2018-10-30 2021-12-07 Nuvation Bio Inc. Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors
WO2020127846A1 (en) * 2018-12-21 2020-06-25 Albert Ludwig Universität Freiburg Condensed pyrroles as novel bromodomain inhibitors
CA3145827A1 (en) * 2019-07-02 2021-01-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
CN110272418B (en) * 2019-07-25 2020-10-16 山东大学 Triazole compound and preparation method and application thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022033542A1 (en) * 2020-08-14 2022-02-17 南京明德新药研发有限公司 5-membered heteroaromatic pyridone compounds and application thereof
CN114808429A (en) * 2022-03-23 2022-07-29 王树芹 Elastic wrinkle-free fabric and preparation method thereof

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1446153A (en) * 1974-03-20 1976-08-18 Lepetit Spa Pyrrolo-3,4-d-pyrimidines and methods for their preparation
GB1447426A (en) * 1974-03-20 1976-08-25 Lepetit Spa Pyrrolo 3,4-d- pyrimidines and methods for their preparation
US6630476B2 (en) * 2000-07-07 2003-10-07 Bristol-Myers Squibb Pharma Company Pyrrolo [3,4-d] pyrimidines as corticotropin releasing factor (CRF) antagonists
US8117844B2 (en) * 2004-05-07 2012-02-21 Recurrent Engineering, Llc Method and apparatus for acquiring heat from multiple heat sources
TWI447120B (en) 2005-05-30 2014-08-01 Mitsubishi Tanabe Pharma Corp Thienotriazolodiazepine compound and a medicinal use thereof
WO2008024978A2 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
DK2722334T3 (en) 2009-11-05 2016-03-07 Glaxosmithkline Llc benzodiazepine bromdomæneinhibitor
EP2585465B1 (en) * 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
WO2012075456A1 (en) * 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
GB201106799D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
EP2705039B1 (en) * 2011-05-04 2017-07-26 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201107325D0 (en) * 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
WO2012174487A2 (en) * 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) * 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors

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